C5-PIPERAZINYL-1,4-BENZODIAZEPINES, WATER-SOLUBLE, ORALLY BIOAVAILABLE CCKB GASTRIN RECEPTOR ANTAGONISTS

Authors
SHOWELL GA BOURRAIN S FLETCHER SR NEDUVELIL JG FLETCHER AE FREEDMAN SB PATEL S SMITH AJ MARSHALL GR GRAHAM MI SOHAL B MATASSA VG
Citation
Ga. Showell et al., C5-PIPERAZINYL-1,4-BENZODIAZEPINES, WATER-SOLUBLE, ORALLY BIOAVAILABLE CCKB GASTRIN RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 5(24), 1995, pp. 3023-3026
Citations number
11
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
24
Year of publication
1995
Pages
3023 - 3026
Database
ISI
SICI code
0960-894X(1995)5:24<3023:CWOB>2.0.ZU;2-O
Abstract
A novel series of potent, water-soluble benzodiazepine based CCKB/gast rin antagonists has been prepared which incorporate an N-methylpiperaz ine group at the C5 position of the benzodiazepine ring system. The N1 -n-propyl analogue (7b) is a high affinity, selective and potent recep tor antagonist in vitro, with good bioavailability and excellent oral absorption providing high plasma levels in vivo.